FIELD: organic chemistry, medicine, pharmacy. SUBSTANCE: invention relates to novel carboxy-substituted cyclic derivatives of carboxamide of the formula (I): where G1 means CH2; G2 means C(O); m = 2 or 3; n = 0 or 1; R1 means 1-3 substitutes taken independently among H, halogen, C1-C6-alkoxy-group; R2 means 1-3 substituted taken independently among H, C1-C6-alkoxy-group; R3 means H or ; R4 means H; Ar1 means and ; R8 means 1-3 substitutes taken independently among H, halogen; R9 means ; A means where p = 1, 2, 3 or 4; X means -O-, -CH2-; R10 means H, C1-C6/ -alkyl or where q = 2 or 3; R5 means C1-C4-alkyl, (CH2)2OH; R6 means C1-C4-alkyl, -(CH2)2OH, (CH2)2N(CH3)2;; means C1-C4-alkyl; R7 means C1-C6-alkyl and its stereoisomers and pharmaceutically acceptable salts. Invention describes method of their synthesis also. Compounds of the formula (I) elicit antagonistie activity with respect to receptors NK1 and NK2 that allows to use their in pharmaceutical composition for treatment of patients with asthma, cough and bronchitis. EFFECT: improved method of synthesis, valuable medicinal properties of compounds. 69 cl, 2 sch, 1 tbl, 38 ex
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Authors
Dates
2003-02-27—Published
1997-11-21—Filed